Synthesis and structure–activity relationships of a new class of 1-oxacephem-based human chymase inhibitors

1-Oxacephem derivatives were synthesized and evaluated as a novel series of chymase inhibitors. Structure–activity relationship studies of 1-oxacephems led to compound 34, which exhibited 6 nM inhibition of human chymase and high selectivity for human chymase compared to other serine enzymes.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-11, Vol.10 (21), p.2397-2401
Main Authors: Aoyama, Yasunori, Uenaka, Masaaki, Konoike, Toshiro, Iso, Yasuyoshi, Nishitani, Yasuhiro, Kanda, Akiko, Naya, Noriyuki, Nakajima, Masatoshi
Format: Article
Language:English
Subjects:
Biological and medical sciences
Cardiovascular system
Cephalosporins - chemical synthesis
Cephalosporins - chemistry
Cephalosporins - pharmacology
Chymases
Drug Design
Humans
Medical sciences
Miscellaneous
Molecular Structure
Pharmacology. Drug treatments
Serine Endopeptidases - chemistry
Serine Endopeptidases - metabolism
Serine Proteinase Inhibitors - chemical synthesis
Serine Proteinase Inhibitors - chemistry
Serine Proteinase Inhibitors - metabolism
Serine Proteinase Inhibitors - pharmacology
Structure-Activity Relationship
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Summary:1-Oxacephem derivatives were synthesized and evaluated as a novel series of chymase inhibitors. Structure–activity relationship studies of 1-oxacephems led to compound 34, which exhibited 6 nM inhibition of human chymase and high selectivity for human chymase compared to other serine enzymes.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00488-1